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BİNGÖL ÖZAKPINAR, ÖZLEM

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BİNGÖL ÖZAKPINAR

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ÖZLEM

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2013 - 20172
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Author: ÖZSAVCI, DERYA × Subject: anticancer ×

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Now showing 1 - 2 of 2
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    PublicationOpen Access
    Synthesis and Characterization of Celecoxib Derivatives as Possible Anti-Inflammatory, Analgesic, Antioxidant, Anticancer and Anti-HCV Agents
    (MDPI, 2013-03-21) ŞENER, AZİZE; Kucukguzel, S. Guniz; Coskun, Inci; Aydin, Sevil; Aktay, Goknur; Gursoy, Sule; Cevik, Ozge; Ozakpinar, Ozlem Bingol; Ozsavci, Derya; Sener, Azize; Kaushik-Basu, Neerja; Basu, Amartya; Talele, Tanaji T.
    A series of novel N-(3-substituted aryl/alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamides 2a-e were synthesized by the addition of ethyl alpha-bromoacetate and anhydrous sodium acetate in dry ethanol to N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)-3-(trifluoro-methyl)- 1H-pyrazol-1-yl] benzene sulfonamides 1a-e, which were synthesized by the reaction of alkyl/aryl isothiocyanates with celecoxib. The structures of the isolated products were determined by spectral methods and their anti-inflammatory, analgesic, antioxidant, anticancer and anti-HCV NS5B RNA-dependent RNA polymerase (RdRp) activities evaluated. The compounds were also tested for gastric toxicity and selected compound 1a was screened for its anticancer activity against 60 human tumor cell lines. These investigations revealed that compound 1a exhibited anti-inflammatory and analgesic activities and further did not cause tissue damage in liver, kidney, colon and brain compared to untreated controls or celecoxib. Compounds 1c and 1d displayed modest inhibition of HCV NS5B RdRp activity. In conclusion, N-(ethylcarbamothioyl)-4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide (1a) may have the potential to be developed into a therapeutic agent.
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    PublicationOpen Access
    Synthesis, characterization and biological evaluation of thioureas, acylthioureas and 4-thiazolidinones as anticancer and antiviral agents
    (MARMARA UNIV, FAC PHARMACY, 2017-04-01) ÖZSAVCI, DERYA; Kulabas, Necla; Ozakpinar, Ozlem Bingol; Ozsavci, Derya; Leyssen, Pieter; Neyts, Johan; Kucukguzel, Ilkay
    In this study, thiourea derivatives [1-4] were synthesized by using 2-amino-4-substituted pyridine compounds and these compounds have been used as the starting materials for synthesis of 2-imino-1,3-thiazolidin-4-one ring [5, 6]. Two different procedures for 4-thiazolidinone ring closure and synthesis method were optimized. The synthesized compounds were identified by the help of elemental analysis, IR, H-1-NMR, C-13-NMR and mass spectral data while the purities of them were proved with TLC. Synthesized compounds were evaluated for their antiviral and anticancer activity. Antiviral activity against Murine norovirus, Yellow fever, Enterovirus and Chikungunya strains of the test compounds were investigated and EC 50 values of these compounds were determined higher than 0,3 mu M. Cytotoxicity of test compounds was examined on NIH3T3 cell line. When the anticancer activity of test compounds was examined against PC-3, A549, HeLa, HT-29, MCF-7, SJSA1 and K562 cell lines, the percent proliferation values of these compounds were observed over 61% for all cell lines.